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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
19
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pubmed:dateCreated |
2008-10-2
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pubmed:abstractText |
A series of novel biphenyl piperazines was discovered as highly potent muscarinic acetylcholine receptor antagonists via high throughput screening and subsequent optimization. Compound 5c with respective 500- and 20-fold subtype selectivity for M3 over M2 and M1 exhibited excellent inhibitory activity and long duration of action in a bronchoconstriction in vivo model in mice via intranasal administration. The novel inhaled mAChR antagonists are potentially useful therapeutic agents for the treatment of chronic obstructive pulmonary disease.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:BelmonteKristen EKE,
pubmed-author:BerlangaManuelaM,
pubmed-author:BudzikBrianB,
pubmed-author:BurmanMiriamM,
pubmed-author:FoleyJames JJJ,
pubmed-author:KANEG GGG,
pubmed-author:LainéDramane IDI,
pubmed-author:MooreMichael LML,
pubmed-author:MorrowDwight MDM,
pubmed-author:PalovichMichaelM,
pubmed-author:RiveroRalph ARA,
pubmed-author:SalmonMichaelM,
pubmed-author:SarauHenry MHM,
pubmed-author:ShiDongchuanD,
pubmed-author:WanZehongZ,
pubmed-author:WangFengF,
pubmed-author:WangYonghuiY,
pubmed-author:WebbEdward FEF,
pubmed-author:XieHaiboH,
pubmed-author:ZhuChongyeC
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pubmed:issnType |
Electronic
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pubmed:day |
9
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5915-8
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pubmed:meshHeading |
pubmed-meshheading:18798607-Administration, Intranasal,
pubmed-meshheading:18798607-Animals,
pubmed-meshheading:18798607-Bronchial Provocation Tests,
pubmed-meshheading:18798607-Bronchoconstriction,
pubmed-meshheading:18798607-Bronchoconstrictor Agents,
pubmed-meshheading:18798607-Bronchodilator Agents,
pubmed-meshheading:18798607-Disease Models, Animal,
pubmed-meshheading:18798607-Drug Evaluation, Preclinical,
pubmed-meshheading:18798607-Methacholine Chloride,
pubmed-meshheading:18798607-Mice,
pubmed-meshheading:18798607-Molecular Structure,
pubmed-meshheading:18798607-Piperazines,
pubmed-meshheading:18798607-Receptors, Muscarinic,
pubmed-meshheading:18798607-Stereoisomerism,
pubmed-meshheading:18798607-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.
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pubmed:affiliation |
GlaxoSmithKline, 709 Swedeland Road, King of Prussia, Pennsylvania 19406, USA. jianjin@unc.edu
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pubmed:publicationType |
Journal Article
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